6-Aryl-quinazolines as novel GABAB receptor positive allosteric modulators

被引：1

作者：

Huszar, Jozsef ^{[1
]}

Petro, Jozsef Levente ^{[1
]}

Hadady, Zsuzsa ^{[1
]}

Bobok, Amrita Agnes ^{[1
]}

Saghy, Katalin ^{[1
]}

Halasz, Attila Sandor ^{[1
]}

Hornyanszky, Gabor ^{[2
]}

Roman, Viktor ^{[1
]}

Greiner, Istvan ^{[1
]}

Eles, Janos ^{[1
]}

机构：

[1] Chem Works Gedeon Richter Plc, 30-32 Gyomro St, H-1103 Budapest, Hungary

[2] Budapest Univ Technol & Econ, Dept Organ Chem & Technol, 8 Budafok St, H-1111 Budapest, Hungary

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2022年 / 67卷

关键词：

-Aminobutyric acid; GABA; GABA B receptor; Positive allosteric modulators; PAMs; GS39783; CGP7930; BACLOFEN; AGONISTS;

D O I：

10.1016/j.bmcl.2022.128714

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The systemic use of GABAB orthosteric agonist baclofen might be limited due to its detrimental properties: sedation and motor impairment. In contrast, GABAB positive allosteric modulators produce less adverse effects. Using BHF-177 as a starting point, we found a new active scaffold: the 6-aryl-quinazoline scaffold. Further elaborating the scaffold, we identified several in vitro and in vivo active compounds.

引用

页数：4

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